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Titolo:
ETHANOL INHIBITION OF NICOTINIC ACETYLCHOLINE TYPE ALPHA-7 RECEPTORS INVOLVES THE AMINO-TERMINAL DOMAIN OF THE RECEPTOR
Autore:
YU DH; ZHANG L; EISELE JL; BERTRAND D; CHANGEUX JP; WEIGHT FF;
Indirizzi:
NIAAA,LMCN,NIH,12501 WASHINGTON AVE ROCKVILLE MD 20852 NIAAA,LMCN,NIH ROCKVILLE MD 20852 INST PASTEUR,UR D1284 CNRS F-75724 PARIS 15 FRANCE CTR MED UNIV GENEVA,DEPT PHYSIOL,FAC MED CH-1211 GENEVA 4 SWITZERLAND
Titolo Testata:
Molecular pharmacology
fascicolo: 4, volume: 50, anno: 1996,
pagine: 1010 - 1016
SICI:
0026-895X(1996)50:4<1010:EIONAT>2.0.ZU;2-U
Fonte:
ISI
Lingua:
ENG
Soggetto:
GATED ION-CHANNEL; POTASSIUM CHANNEL; LIGAND-BINDING; ALCOHOLS; POTENTIATION; ANESTHETICS; ENDPLATE; PROTEIN; OOCYTES; CLONING;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
35
Recensione:
Indirizzi per estratti:
Citazione:
D.H. Yu et al., "ETHANOL INHIBITION OF NICOTINIC ACETYLCHOLINE TYPE ALPHA-7 RECEPTORS INVOLVES THE AMINO-TERMINAL DOMAIN OF THE RECEPTOR", Molecular pharmacology, 50(4), 1996, pp. 1010-1016

Abstract

Recent studies have suggested that alcohols can affect the function of neuro transmitter-gated ion channels by a direct interaction with the receptor protein. However, the molecular region of the receptor protein that mediates the alcohol action is not known. To address this question, we studied the effect of ethanol on the function of recombinantnicotinic acetylcholine type alpha 7 (nACh(alpha 7)) receptors, 5-hydroxytryptamine (serotonin) type 3 (5-HT3) receptors, and a chimeric receptor constructed from these two receptors. The receptors were expressed in Xenopus oocytes and their function was studied using the two-electrode voltage-clamp technique. Ethanol inhibited the response of nACh(alpha 7) receptors in a concentration-dependent manner over the concentration range of 5-100 mM; the EC(50) for this inhibition was 33 mM ethanol. Ethanol decreased the maximal amplitude (E(max)) of the nACh(alpha 7) receptor agonist concentration-response curve, without significantly affecting the EC(50). In contrast, ethanol potentiated 5-HT3 receptor-mediated responses at low agonist concentrations. The potentiation was concentration-dependent over the concentration range of 10-100 mM; the EC(50) for this potentiation was 57 mM ethanol. The magnitude of the ethanol potentiation of 5-HT3 receptor-mediated responses decreased with increasing agonist concentration. The chimeric receptor had the amino-terminal domain from the nACh(alpha 7) receptor and the transmembrane and carboxyl-terminal domains from the 5-HT3 receptor. Ethanol was found to inhibit the function of this chimeric receptor in a manner similar to that of nACh(alpha 7) receptors. Because the inhibition transfers with the amino-terminal domain of the receptor, the observations suggest that the amino-terminal domain of the receptor is involved in the inhibition.

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Documento generato il 21/09/20 alle ore 18:51:02